2-Amino-5-phosphonovalerate (2APV), a potent and selective antagonist of amino acid-induced and synaptic excitation

Abstract

A new compound, 2-amino-5-phosphonovaleric acid (2APV) is the most potent and selective N-methyl-D-aspartate (NMDA) receptor antagonist yet tested. As with other compounds of this type, it blocks L-aspartate and dorsal root-evoked excitation of spinal neurons, but is without effect on the cholinergic excitation of Renshaw cells evoked by exogenous acetylcholine or ventral root stimulation. The high potency and selectivity of this compound should prove to be of great value in investigations of the amino acid receptor types involved in synaptic excitation.